Flavonoids are the natural phytoconstituents recognized as secondary metabolites of plant, with marked biological significance such as Anti-inflammatory, Antioxidant, Anticancer and Antimicrobial activity. After the cardiovascular diseases, cancer is the second most common cause of death. Aromatase enzyme is mainly involved in the conversion of androgens to estrogen. In post-menopausal female, Aromatase enzyme is mostly localized in breast tumor. After skin cancer, breast cancer is most common in women. This work deals with a molecular docking study of novel flavones derivatives was performed by using Schrodinger (Maestro 11.5v) with PDB Id: 3EQM for drug protein interaction study. The main objective of molecular docking is to predict the biological activity of given ligand. On the basis of docking study the ligand protein interaction diagram shows that the flavones interacted with ARG115, LEC477 and MET374 the most active binding site of an aromatase enzyme. Compounds (c, f, h, k) derivatives were most active with (-8.286, -7.923, -8.056, -8.000) docking score and (-8.286, -7.943, -8.078, -8.112) Glide score respectively comparatively higher than standard (Fadrozole) Docking Score (-7.564) and standard Glide Score (-7.725). It was demonstrated that the docking practice could reliably reproduce the interaction of aromatase with its substrate. The insights gained from the study herein have great potential for the design of novel flavones as Aromatase Inhibitors.
Moisture activated dry granulation technique is the novel method which increases the commercial aspects and Zolpidem tartrate. The selected drug candidate belongs to the category of Sedative and hypnotic and used for the treatment of insomnia. The aim of the present study was to design Zolpidem tartrate tablets by moisture activated dry granulation technique. Zolpidem tartrate tablets were prepared by using Lactose monohydrate as diluent, microcrystalline cellulose as moisture absorbing agent and magnesium stearate as lubricant. The granules prepared by varying the concentration (1%, 2%, 4%, 6%, 7% 10%) of water and granules were subjected for pre formulation studies (angle of repose, bulk density, tapped density, particle size distribution, compressible index and Hausner’s ratio). The prepared granules were subjected for compression and the tablets were subjected for post formulation studies (thickness, weight variation, hardness, friability, disintegration, drug content, dissolution study). The Zolpidem tartrate tablets release profile was carried by using water as the dissolution medium. The prepared granules and tablets are compared to the Zolpidem tartrate granules and tablets prepared by using wet granulation technique (10% concentration of water). Among all the formulations 5% concentration of water is concluded as best formulation by comparing with wet granulated formulation.
K. Mary Swarna Latha*, B. Sowjanya, K. Abbulu, E. Pushpa latha.
Brassica nigra are the species of Brassica genus (Family: Brassicaceae). The foregoing study showed that Brassica nigra possesses antioxidant, anti-inflammatory, antiepileptic, antidiabetic and many other pharmacological effects. This review will emphasize the chemical constituents and pharmacological effect of the plant.
The oral bioavailability of poorly water soluble drug can be enhanced using nanosuspension. Nanosuspensions are colloidal dispersion of uniform-sized solid particles dispersed in an aqueous vehicle. The present work is aimed at the development and evaluation of nanosuspension of apremilast, a poorly water soluble antipsoratic drug. The nanosuspension of apremilast may enhance the dissolution rate of drug to improve its oral bioavailability. The nanosuspensions were prepared by using high pressure homogenization. The prepared nanosuspensions were evaluated for particle size, zeta potential, polydispersity index. The effect of variable concentration of drug and stabilizer and solvent to antisolvent ratio on the physical, morphological and dissolution properties of apremilast were studied. The average particle size of apremilast nanoparticles was found to be in the range of 399 nm. The particle size varies with increase in concentration of drug and stabiliser. The nanosuspension showed negative zeta potential i.e. about -14.1. The dissolution proļ¬les of nanosuspension formulation showed up to 98.34% release in 6 h. The prepared nanosuspension showed enhanced dissolution which may lead to enhanced oral bioavailability of apremilast.
A vast majority of heterocyclic derivatives containing oxygen and nitrogen have been used as versatile scaffolds in drug development. Furoxan is a five-membered nitrogen and oxygen containing ring with two active oxygen atoms. Furoxan (1,2,5-oxadiazole 2-oxide) are very important scaffold in medicinal chemistry as NO donors, which releases high levels of NO in vitro. Compounds containing furoxan ring show a variety of biological activities. Due to its potent and significant biological activities it has great pharmaceutical importance; hence, synthesis of this compound is of considerable interest. This review work focuses on the research work reported in the scientific literature on Furoxan compounds.
Pravin R. Dighe*, Amol S. Deshmukh, Suvarna J. Shelke.